LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
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LDN193189 Chemical Structure
CAS No. : 1062368-24-4
This product is a controlled substance and not for sale in your territory.
Based on 52 publication(s) in Google Scholar
Other Forms of LDN193189:
LDN193189 Tetrahydrochloride
In-stock
LDN-193189 dihydrochloride
In-stock
LDN193189 (GMP)
In-stock
LDN193189 purchased from MedChemExpress. Usage Cited in:
Oxid Med Cell Longev. 2020 Jun 8;2020:4175613.
[Abstract]
Western blot and grey analysis of CYP11a1, CYP19a1, BCL2, CALR, CHOP, caspase3, caspase12, PERK, and GRP78. qRT-PCR analyzed ATF4, caspase3, and GRP78 mRNAs. The relieving function of BMP4 on ER stress is diminished after blockade of BMP receptor I (BMPRI) with DM-3189.
H9c2 cells are treated as following: control, DOX, DOX + rhBMP (Bmpr1a agonist) and DOX + LDN193189 (Bmpr1a inhibitor). Cells with red fluorescence indicate favorable MMP while green fluorescence indicates damage.
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Description
LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva[1][2][3].
IC50 & Target[1]
ACVR1
5 nM (IC50)
BMPR1A
30 nM (IC50)
In Vitro
LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively[1].
LDN-193189 has weake effects on activin and the TGF-β type I receptors ALK4, ALK5 and ALK7 with IC50 values of ≥ 500 nM[1].
LDN-193189 binds ActRIIA with Kd value of 14 nM[2].
LDN-193189 (0.5 μM; 30 min) targets GDF8 induced Smad2/3 signaling and repression of myogenic transcription factors[2].
LDN-193189 (0.05, 0.5, 5 μM) efficiently inhibits GDF8 induced Smad3/4 reporter gene activity[2].
LDN-193189 (0-5 μM) rescues myogenesis in myoblasts treated with GDF8[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
LDN193189 Related Antibodies
Western Blot Analysis[2]
Cell Line:
Primary human myoblasts, C2C12 cells
Concentration:
0.5 μM
Incubation Time:
30 min
Result:
Inhibited GDF8-induced signaling pathways in undifferentiated and in differentiated primary human myoblasts and in C2C12 premyoblasts.
In Vivo
LDN-193189 (i.p.; 3 mg/kg; daily; for 35 days) might affect the interaction between breast cancer cells and the bone environment[3].
LDN-193189 (i.p.; 3 mg/kg; single) shows a reduction in ectopic ossification and functional impairment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Ahymic NMRI nude female mice (6-week-old)[3]
Dosage:
3 mg/kg
Administration:
Itraperitoneal, daily, for 35 days
Result:
Ehanced etastases development in vivo.
Animal Model:
C57BL/6 mice[1]
Dosage:
3 mg/kg
Administration:
Intraperitoneal, single
Result:
Diminished ectopic bone formation and preserved joint spaces over the same interval without inducing fractures, osteopenia or skeletal abnormalities.
Room temperature in continental US; may vary elsewhere.
Stockage
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
2 years
-20°C
1 year
Solvant et solubilité
In Vitro:
DMSO : 10 mg/mL (24.60 mM; ultrasonic and warming and adjust pH to 2 with 1M HCl and heat to 80°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
Preparing Stock Solutions
ConcentrationSolventMass
1 mg
5 mg
10 mg
1 mM
2.4601 mL
12.3007 mL
24.6015 mL
5 mM
0.4920 mL
2.4601 mL
4.9203 mL
10 mM
0.2460 mL
1.2301 mL
2.4601 mL
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 1 mg/mL (2.46 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 1 mg/mL (2.46 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 1 mg/mL.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.
[Content Brief]
[2]. Daniel Horbelt, et al. Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation. J Biol Chem. 2015 Feb 6;290(6):3390-404.
[Content Brief]
[3]. Julien Vollaire, et al. The Bone Morphogenetic Protein Signaling Inhibitor LDN-193189 Enhances Metastasis Development in Mice. Front Pharmacol. 2019 Jun 19;10:667.
[Content Brief]
[1]. Yu PB, et al. BMP type I receptor inhibition reduces heterotopic [corrected] ossification. Nat Med, 2008, 14(12), 1363-1369.
[2]. Daniel Horbelt, et al. Small molecules dorsomorphin and LDN-193189 inhibit myostatin/GDF8 signaling and promote functional myoblast differentiation. J Biol Chem. 2015 Feb 6;290(6):3390-404.
[3]. Julien Vollaire, et al. The Bone Morphogenetic Protein Signaling Inhibitor LDN-193189 Enhances Metastasis Development in Mice. Front Pharmacol. 2019 Jun 19;10:667.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
2.4601 mL
12.3007 mL
24.6015 mL
61.5036 mL
5 mM
0.4920 mL
2.4601 mL
4.9203 mL
12.3007 mL
10 mM
0.2460 mL
1.2301 mL
2.4601 mL
6.1504 mL
15 mM
0.1640 mL
0.8200 mL
1.6401 mL
4.1002 mL
20 mM
0.1230 mL
0.6150 mL
1.2301 mL
3.0752 mL
LDN193189 Related Classifications
Stem Cell/WntTGF-beta/Smad
OrganoidTGF-β Receptor
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
Keywords:
LDN1931891062368-24-4DM-3189LDN 193189LDN-193189DM3189DM 3189OrganoidTGF-β ReceptorTransforming growth factor beta receptorsbone morphogenetic protein (BMP)BMP I receptortranscriptionALK2ALK3bone morphogenetic protein signallingfibrodysplasia ossificans progressivaInhibitorinhibitorinhibit
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